| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 161 | 광학이성적으로 농축된 기질의 탈농축 방법 | KR1020077009554 | 2005-10-27 | KR1020070068428A | 2007-06-29 | 블랙커,앤드류,존; 스터링,매튜,존 |
| There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group VI heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or disatereomer in the product composition being greater than the ratio of second to first enantiomer or disatereomer in the enantiomerically enriched composition. Preferred substrates include compounds of Formula (1) wherein: X represents O, S; R1, R2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group; or R1 & R2 are optionally linked in such a way as to form an optionally substituted ring(s); provided that R1 and R2are selected such that * is a chiral centre. In a preferred process a compound of Formula : (2) wherein: X represents O, S; R1, R2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group; or R1 & R2 are optionally linked in such a way as to form an optionally substituted ring(s); provided that R1 and R2 are different, may be obtained. | ||||||
| 162 | 인테그린 길항물질과 20 번 위치에서 공액된7-티-부톡시이미노메틸캄토테신 | KR1020067025046 | 2005-04-28 | KR1020070022290A | 2007-02-26 | 달포쪼,알마; 펜코,세르지오; 메를리니,루치오; 지아니니,지우세페; 틴티,마리아,오르넬라; 피사노,클라우디오; 주니노,프랑코; 알로아티,도메니코; 베쉬,로레다나; 달라발레,사브리나; 니밍홍 |
| R1 그룹이 명세서에서 정의한 바와 같고 20 번 위치에서, RGD 서열을 함유하는 사이클로펩티드와 7-t-부톡시이미노메틸캄토테신과의 축합을 포함하는 화학식 I의 화합물을 개시한다. 상기 화합물은 인테그린 수용체 α v ß 3 및 α v ß 5 에 대한 높은 친화성과 마이크로 몰 농도에서 인간 종양 세포 주에 대해 선택적인 세포독성 활성을 모두 갖는다. [화학식 I] 사이클로펩티드, 7-t-부톡시이미노메틸캄토테신, 축합, 인테그린 수용체 | ||||||
| 163 | 레보부피바카인및그의유사체의제조에사용하는라세미화및비대칭변환방법 | KR1019970701774 | 1995-09-22 | KR100393133B1 | 2003-11-17 | 다이어울리치콘라드; 록크크리스토퍼제임스; 우즈마틴 |
| PCT No. PCT/GB95/02247 Sec. 371 Date May 30, 1997 Sec. 102(e) Date May 30, 1997 PCT Filed Sep. 22, 1995 PCT Pub. No. WO96/09290 PCT Pub. Date Mar. 28, 1996A process for the racemisation of an optically-enriched piperidine-2-carboxanilide compound, comprises heating the compound in the presence of an alkanoic or arylalkanoic acid. A process for the asymmetric transformation of such a compound comprises heating the compound in the presence of an acid as defined above, a chiral acid resolving agent and an inert cosolvent. | ||||||
| 164 | (알)-(-)-무스콘의 입체선택적 제조 방법 | KR1020000023417 | 2000-05-02 | KR1020000049811A | 2000-08-05 | 김용해; 최용현; 김권 |
| PURPOSE: A stereo-selective method for preparing (R)-(-)-muscone with high optical purity and high yield is provided. CONSTITUTION: A method for preparing (R)-(-)-muscone comprises steps of: (i) reacting 4-(cis-2, 6-dimethylpiperidine)-(R)-dinaphtodioxaphosphepin of the following formula (I) and 4-(R, R-2, 5-diphenylpyrrolidine)-(R)-dinaphtodioxaphosphepin of the following formula (II) with Cu(OTf)2 to form a complex with copper; and (ii) 1, 4-addition reacting dimethylzinc with 2-cyclopentadecenone using the complex of step (i) as a chiral catalyst. | ||||||
| 165 | PRODUCTION METHOD FOR RACEMATE OF COMPOUND | EP13851011.0 | 2013-10-28 | EP2915801B1 | 2018-07-04 | TAKAHASHI, Tomoaki; HIROSE, Taro |
| A method for producing a racemate of a compound represented by Formula (1), including bringing a transition metal catalyst into contact with an optically active form of the compound represented by Formula (1) : [in Formula (1), a ring X 1 represents an aromatic ring; R 1 represents a C 1-6 alkyl group, a C 3-8 cycloalkyl group, or a C 1-6 halo-alkyl group; R 2 is a group different from R 1 and represents a C 1-6 alkyl group, a C 3-8 cycloalkyl group, or a C 1-6 halo-alkyl group, or R 2 and the ring X 1 are bonded to each other to form a ring; a hydrogen atom(s) of the ring X 1 is optionally replaced with a C 1-6 alkyl group, a C 1-6 halo-alkyl group, a cyano group, a nitro group, a C 1-6 alkoxy group, or a halogen atom; and * represents an asymmetric carbon atom]. | ||||||
| 166 | VERFAHREN ZUR HERSTELLUNG EINES GEMISCHES VON LACTID-DERIVATEN | EP09778182.7 | 2009-08-28 | EP2321294B1 | 2015-09-30 | HAGEN, Rainer; VERWEIJ, Adam, Bastiaan; MÜHLBAUER, Udo; SCHULZE, Joachim; TIETZ, Wolfgang; GÖHLER, Klaus-Dieter |
| 167 | Verfahren zur Herstellung eines Gemisches von Lactid-Derivaten | EP11004941.8 | 2009-08-28 | EP2392570B1 | 2014-10-01 | Hagen, Rainer; Verweij, Adam Bastiaan; Mühlbauer, Udo; Schulze, Joachim; Tietz, Wolfgang; Göhler, Klaus-Dieter |
| 168 | PROCESS FOR PRODUCING -SUBSTITUTED ESTER | EP09826005 | 2009-10-22 | EP2357164A4 | 2014-05-07 | AKIHIRO ISHII; MANABU YASUMOTO |
| 169 | Process of separating chiral isomers of chroman compounds and their derivatives and precursors | EP11165442.2 | 2011-05-10 | EP2522647B1 | 2014-04-30 | Schiefer, Gerhard; Netscher, Thomas; Duchateau, Alexander Lucia, Leonardus |
| 170 | PROCESS FOR PRODUCING ALPHA-FLUORO-BETA-AMINO ACIDS | EP09738726.0 | 2009-04-21 | EP2246322B1 | 2013-04-03 | Akihiro ISHII; Takako YAMAZAKI; Manabu YASUMOTO; Takashi MASUDA; Hideyuki TSURUTA |
| 171 | Process of separating chiral isomers of chroman compounds and their derivatives and precursors | EP11165442.2 | 2011-05-10 | EP2522647A1 | 2012-11-14 | The designation of the inventor has not yet been filed |
The present invention relates to a process of separating chiral isomers of chroman compounds, particularly tocopherols and tocotrienols as well as the esters and intermediates thereof. It has been found that this process allows a separation of the desired isomer with a higher yield and enables the use of the non-desired isomers in a very efficient way. Said process is particularly useful when implemented in an industrial process. Furthermore, it has been found that this process allows using isomer mixtures as they result from traditional industrial synthesis. |
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| 172 | METHOD FOR PRODUCING OPTICALLY ACTIVE DIAMINE DERIVATIVE | EP10750859 | 2010-03-10 | EP2407450A4 | 2012-08-01 | KAWANAMI KOUTAROU |
| 173 | PROCESS FOR PRODUCING -SUBSTITUTED ESTER | EP09826005.2 | 2009-10-22 | EP2357164A1 | 2011-08-17 | Akihiro, ISHII; Manabu YASUMOTO |
There is provided a process for producing an α-substituted ester by reaction of a fluorosulfuric acid ester of α-hydroxyester with a Grignard reagent in the presence of a zinc catalyst. It is newly found that the reaction for production of α-substituted esters, in which the raw reaction substrate is limited to expensive trifluoromethanesulfonic acid esters, can proceed favorably with the use of fluorosulfuric acid esters suitable for mass-production uses. By the use of the fluorosulfuric acid ester high in optical purity, it is possible to obtain the α-substituted ester with high optical purity upon inversion of the asymmetric carbon configuration. The process of the present invention can solve all of the prior art problems and can be applied for industrial uses. |
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| 174 | PROCESS FOR THE MANUFACTURE OF RACEMIC 2-ARYL-PROPIONIC ACID | EP09772783.8 | 2009-06-30 | EP2307335A1 | 2011-04-13 | MARTIN, Stephen, John; MAKIN, Scott, Dale |
| There is described a process for the manufacture of a racemic 2-aryl propionic acid compound, or a pharmaceutically acceptable salt thereof, which comprises reacting the S- or R- enantiomer of the corresponding 2-aryl propionic acid compound with a base. | ||||||
| 175 | Chiral binaphtol derivatives as alanine racemase mimics with powerful hydrogen bond donors: their use for optical resolution and optical inversion | EP10156417.7 | 2008-02-07 | EP2189433A1 | 2010-05-26 | Kim, Kwan Mook.; Tang, Lijun. |
Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided. |
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| 176 | METHOD FOR CRYSTALLISATION FROM A SOLUTION | EP08775431.3 | 2008-06-04 | EP2169094A1 | 2010-03-31 | OSUNA ESTEBAN, Susana; ZORZANO MIER, Mª, Paz; MENOR SALVÁN, Cesar; RUIZ BERMEJO, Marta; VEINTEMILLAS VERDAGUER, Sabino |
The present invention relates to a novel method and to a device for obtaining crystals from a substance, comprising: (i) preparing a saturated dissolution of the substance to be crystallized in a suitable solvent in a reaction vessel; (ii) generating an aerosol in the reaction vessel; (iii) crystallizing the substance; and (iv) recovering the crystals at the bottom of the reaction vessel. The method is especially suitable for crystallizing substances which are typically difficult to crystallize and can lead to a chiral amplification result. |
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| 177 | PROCESS FOR THE RACEMIZATION OF ALCOHOLS | EP02758335.0 | 2002-07-11 | EP1406853A1 | 2004-04-14 | RIERMEIER, Thomas; GROSS, Peter; HOFF, Manfred; MONSEES, Axel; DINGERDISSEN, Uwe |
| A process for the racemization of alcohols using a mixture of ruthenium complexes with chelating N-donor ligands as catalyst precursor and its use in dynamic kinetic resolution of racemates are described. | ||||||
| 178 | PROCESS FOR PRODUCING (8- CHLORO-3,10- DIBROMO-6,11- DIHYDRO- 5H-BENZO 5,6]CYCLOHEPTA 1,2-B]PYRIDIN-11-YL)- 1-PIPERIDINE | EP99931864.5 | 1999-07-01 | EP1091954A1 | 2001-04-18 | NJOROGE, F., George; VIBULBHAN, Bancha; GIRIJAVALLABHAN, Viyyoor, M. |
| A process for producing compounds of formula (1.0) is disclosed. The compound of formula (1.0) is produced by: (1) separating the atropisomers of (2.0) to obtain the atropisomers (2.0A) and (2.0B); (2) heating the atropisomer of formula (2.0B) at a suitable temperature in a suitable solvent to obtain a mixture of atropisomers of formulas (2.0A) and (2.0B); (3) separating the atropisomers of formulas (2.0A) and (2.0B) of step (2); and (4) reducing the atropisomer of formula (2.0A) to obtain a compound of formula (1.0). Preferably, R1 is Br, R2 is Cl and R3 is Br. Also disclosed is the (+)-atropisomer of formula (2.0) wherein R1 is Br, R2 is Cl and R3 is Br. | ||||||
| 179 | RACEMISATION OF QUATERNARY CHIRAL CENTERS | EP97904518.0 | 1997-02-10 | EP0880497A1 | 1998-12-02 | McCAGUE, Raymond |
| A process for the racemisation of an enantiomerically-enriched compound of the formula (3): X-(Ar)(Ak)C-(CH2)2-Y, comprises treatment of enantiomerically-enriched (3) with a base to obtain anion (4), optionally in protonated form, which is then combined with CH2=CH-Y1 to form racemic (3), wherein Ar = aryl or heteroaryl; Ak = C¿1-20? alkyl; X = CN, CO2R, CONR?1R2¿, COR; Y and Y1 are independently selected from CN, CO¿2?R, CONR?1R2¿ and COR; and R, R¿1? and R2 are independently selected from H and C1-20 alkyl; optionally as a salt thereof. This racemisation process can be used as part of an efficient synthesis of enantiomerically-enriched verapamil or aminoglutethimide. | ||||||
| 180 | RACEMISATION OF PRECURSORS TO LEVOBUPIVACAINE AND ANALOGUES THEREOF | EP95933510.0 | 1995-10-09 | EP0784603A2 | 1997-07-23 | DYER, Ulrich, Conrad, Chiroscience Limited; McCAGUE, Raymond; WOODS, Martin, Chiroscience Limited |
| A process for the preparation of optically-enriched pipecolic acid as a salt with an optically-active acid, comprises asymmetric transformation of pipecolic acid, as a racemic mixture or a mixture enriched in the opposite enantiomer from that desired, with the optically-active acid in a solvent comprising an acid that causes racemisation, in the absence of aldehyde. | ||||||
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